Cholecystokinin-1 Receptor

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Encyclopedia of Signaling Molecules
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Synonyms

CCK(A) receptor; CCK1; CCK-A receptor; CCKA; CCKAR; CCK-AR; Cholecystokinin receptor 1; Cholecystokinin type A receptor; Cholecystokinin-1 receptor; CCK-1 receptor; Peripheral type CCK receptor

Historical Background

The hormone cholecystokinin (CCK) was discovered in 1928 by Ivy and Oldberg, based on its ability to stimulate gallbladder contraction. Fifteen years later, Harper and Raper described a factor capable of stimulating pancreatic exocrine secretion (pancreozymin). When Jorpes and Mutt finally isolated the CCK peptide from porcine duodenum in 1966, it became clear that this single hormone was responsible for both of these classical physiological gastrointestinal regulatory activities. Many years later, in 1992, the receptor mediating these effects was finally identified and characterized as a family A guanine nucleotide-binding protein (G protein)-coupled receptor, the CCK-1 receptor (Liddle 1994). Of interest, the cDNA encoding this receptor was initially cloned and...

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References

  • Cawston EE, Miller LJ. Therapeutic potential for novel drugs targeting the type 1 cholecystokinin receptor. Br J Pharmacol. 2010;159:1009–21. PMID: 22467877.

    Article  CAS  PubMed  Google Scholar 

  • Cawston EE, Lam PC, Harikumar KG, Dong M, Ball AM, Augustine ML, Akgün E, Portoghese PS, Orry A, Abagyan R, Sexton PM, Miller LJ. Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor. J Biol Chem. 2012;287:18618–35. PMID: 22467877.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Gao F, Sexton PM, Christopoulos A, Miller LJ. Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor. Bioorg Med Chem Lett. 2008;18:4401–4.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Harikumar KG, Cawston EE, Lam PC, Patil A, Orry A, Henke BR, Abagyan R, Christopoulos A, Sexton PM, Miller LJ. Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor. J Biol Chem. 2013;288:21082–95. PMID: 23754289.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Klueppelberg UG, Gates LK, Gorelick FS, Miller LJ. Agonist-regulated phosphorylation of the pancreatic cholecystokinin receptor. J Biol Chem. 1991;266:2403–8.

    CAS  PubMed  Google Scholar 

  • Korner M, Miller LJ. Alternative splicing of pre-mRNA in cancer: focus on G protein-coupled peptide hormone receptors. Am J Pathol. 2009;175:461–72.

    Article  PubMed  PubMed Central  Google Scholar 

  • Liddle RA. Cholecystokinin. In: Walsh JH, Dockray GJ, editors. Gut peptides: biochemistry and physiology. New York: Raven; 1994. p. 175–216.

    Google Scholar 

  • Miller LJ, Gao F. Structural basis of cholecystokinin receptor binding and regulation. Pharmacol Ther. 2008;119:83–95.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Noble F, Wank SA, Crawley JN, Bradwejn J, Seroogy KB, Hamon M, et al. International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol Rev. 1999;51:745–81.

    CAS  PubMed  Google Scholar 

  • Reubi JC, Schaer JC, Waser B. Cholecystokinin(CCK)-A and CCK-B/gastrin receptors in human tumors. Cancer Res. 1997;57:1377–86.

    CAS  PubMed  Google Scholar 

  • Roettger BF, Rentsch RU, Pinon DI, Holicky E, Hadac E, Larkin JM, et al. Dual pathways of internalization of the cholecystokinin receptor. J Cell Biol. 1993;128:1029–41.

    Article  Google Scholar 

  • Sabbatini ME, Bi Y, Ji B, Ernst SA, Williams JA. CCK activates RhoA and Rac1 differentially through Galpha13 and Galphaq in mouse pancreatic acini. Am J Phys. 2010;298:C592–601. PMID: 19940064.

    Article  CAS  Google Scholar 

  • Sayegh AI, Washington MC, Raboin SJ, Aglan AH, Reeve Jr JR. CCK-58 prolongs the intermeal interval, whereas CCK-8 reduces this interval: not all forms of cholecystokinin have equal bioactivity. Peptides. 2014;55:120–5. PMID: 24607725.

    Article  CAS  PubMed  Google Scholar 

  • Whalen EJ, Rajagopal S, Lefkowitz RJ. Therapeutic potential of beta-arrestin- and G protein-biased agonists. Trends Mol Med. 2011;17:126–39.

    Article  CAS  PubMed  Google Scholar 

  • Williams JA. Intracellular signaling mechanisms activated by cholecystokinin-regulating synthesis and secretion of digestive enzymes in pancreatic acinar cells. Annu Rev Physiol. 2001;63:77–97.

    Article  CAS  PubMed  Google Scholar 

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Correspondence to Laurence J. Miller .

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Miller, L.J. (2016). Cholecystokinin-1 Receptor. In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-6438-9_273-1

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  • DOI: https://doi.org/10.1007/978-1-4614-6438-9_273-1

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